Gastrointestinal compositions

Abstract

The invention relates to compositions and methods for treating and/or preventing lower gastrointestinal (GI) disorders in mammalian patients, more particularly for alleviating and/or preventing the lower GI symptoms associated with such disorders.

What is claimed is:  
     
         1 . A composition for treating or preventing gastrointestinal disorders, comprising: 
 a) a safe and effective amount of a GABA analog of the formula selected from the group consisting of:                          and mixtures thereof; and    b) a safe and effective amount of an amino-ether and/or -ester oxide having the formula:                          in which: R 1  is a lower alkyl, R 2  and R 3  which are the same or different are hydrogen or lower alkyl, R 4  is a phenyl or phenoxy nucleus optionally monosubstituted to trisubstituted by substituents which are identical or different, halogen or lower alkoxy, R 5  is a phenyl radical optionally monosubstituted to trisubstituted by substituents which are the same or different, halogen, lower alkyl, lower alkoxy or nitro, a pyridyl radical or a lower alkyl radical, Q is —O— or —COO—, n is equal to zero, 1 or 2, m and q are, independently of one another, equal to zero or to 1, p is an integer ranging from 0 to 9.    
     
     
         2 . A composition according to  claim 1 , further comprising an active is selected from the group consisting of antiinflammatory agents, laxatives, antidiarrheals, antibiotics, antiulceratives, gastric secretion inhibitors, peristalitc stimulants, serotonin (5HT 3 ) receptor antagonists, serotonin (5HT 4 ) receptor agonists, selective serotonin reuptake inhibitors and mixtures thereof.  
     
     
         3 . A composition according to  claim 2 , wherein the serotonin (5HT 4 ) receptor agonist is selected from the group consisting of tegaserod, prucalopride and mixtures thereof.  
     
     
         4 . A composition according to  claim 2 , wherein the selective serotonin reuptake inhibitor is selected from the group consising of fluoxetine, fluvoxamine, paroxetine, sertraline and mixtures thereof.  
     
     
         5 . A composition according to  claim 2 , wherein the laxative is selected from the group consisting of methylcellulose, carboxymehylcellulose sodium, malt soup extract, polyacrylic resin, plantago seeds, dioctyl calcium sulfosuccinate, dioctyl potassium sulfosuccinate, dioctyl sodium sulfosuccinate, mineral oil, magnesium citrate, magnesium hydroxide, magnesium sulfate, dibasic sodium phosphate, monobasic sodium phosphate, sodium biphosphate, glycerin, anthraquinones, diphenylmethanes, castor oil and mixtures thereof.  
     
     
         6 . A composition according to  claim 2 , wherein the antidiarrheal is selected from the group consisting of natural opiates, synthetic opiates, anticholinergics, acetyltannic acid, albumin tannate, alkofanone, aluminum salicylates, catechin, lidamidine, mebiquine, trillium, uzarin and mixtures thereof.  
     
     
         7 . A composition according to  claim 2 , wherein the antiulcerative is selected from the group consisting of aceglutamide aluminum complex, ε-acetamidocaproic acid zinc salt, acetoxolone, arbaprostil, benexate hydrochloride, bismuth subcitrate sol (dried), carbenoxolone, cetraxate, cimetidine, enprostil, esaprazole, famotidine, ftaxilide, gefarnate, guaiazulene, irsogladine, nizatidine, omeprazole, omoprostil, γ-oryzanol, pifarnine, pirenzepine, plaunotol, ranitidine, rioprostil, rosaprostol, rotraxate, roxatidine acetate, sofalcone, spizofurone, sucralfate, teprenone, trimoprostil, thrithiozine, troxipide, zolimidine and mixtures thereof.  
     
     
         8 . A composition according to  claim 2 , wherein the gastric secretion inhibitor is selected from the group consisting of enterogastrone, octreotide and mixtures thereof.  
     
     
         9 . A composition according to  claim 2 , wherein the peristalitc stimulant is selected from the group consisting of metoclopromide, cisapride, domperidone and mixtures thereof.  
     
     
         10 . A composition according to  claim 2 , wherein the serotonin (5HT 3 ) receptor antagonist is selected from the group consisting of renzapride, cilansetron, ondansetron, alosetron and mixtures thereof.  
     
     
         11 . A composition according to  claim 2 , wherein the antibiotic is selected from the group consisting of nitroimidazole antibiotics, tetracyclines, pencillins, cephalosporins, carbopenems, amino-glycosides, macrolide antibiotics, lincosamide antibiotics, 4-quinolones, rifamycins, nitrofurantoin and derivatives of 10-(1-hydroxyethyl)-11-oxo-1-azatricyclo[7.2.0.0.3.8]undec-2-ene-2-carboxylic acid and mixtures thereof.  
     
     
         12 . A composition according to  claim 1 , in the form of a tablet, capsule, microcapsule, suspension, solution, injectable, rectal suppository, rectal cream, rectal ointment, rectal gel.  
     
     
         13 . A composition according to  claim 1 , wherein the amino-ether and/or -ester oxide selected from the group consisting of trimebutine, fedotozine and mixtures thereof.  
     
     
         14 . A composition according to  claim 5 , wherein the laxative is a bulk forming laxative.  
     
     
         15 . A composition according to  claim 14 , wherein the laxative is selected from the group consisting of polycarbophil, calcium polycarbophil and mixtures thereof.  
     
     
         16 . A composition according to  claim 1 , in the form of a tablet, capsule, microcapsule, suspension, solution, injectable, rectal suppository, rectal cream, rectal ointment, rectal gel.  
     
     
         17 . A composition for treating or preventing gastrointestinal disorders, comprising: a GABA analog selected from the group consisting of (1-aminomethyl-3-methylcyclohexyl) acetic acid, (1-aminomethyl-3-methylcyclopentyl)acetic acid, (1-aminomethyl-3,4-dimethylcyclopentyl)acetic acid, 3-(1-aminoethyl)-5-methylhexanoic acid, 3-aminomethyl-5-methyl-hexanoic acid, and (S)-3-(aminomethyl)-5-methylhexanoic acid and mixtures thereof; and an amino-ether and/or -ester oxide selected from the group consisting of trimebutine, fedotozine and mixtures thereof.  
     
     
         18 . A method of treating or preventing gastrointestinal disorders, comprising the step of administering to a mammal in need of such treatment a safe and effective amount of the composition of  claim 1.